63676-25-5
63676-25-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15800 英文別名
LY 117018Ly 139478
Lilly 117018
Phenethipylone
6-Hydroxy-2-(4-hydroxyphenyl)benzo(B)thien-3-yl 4-(2-(1-pyrrolidinyl)ethoxy) phenyl ketone
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone
Methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(B)thien-3-yl)(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-
[6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl][4-[2-(1-pyrrolidinyl)ethoxy]phenyl]methanone
常見問題列表
生物活性
LY117018，Raloxifene 類似物，是一種選擇性雌激素受體 (estrogen receptor) 調(diào)節(jié)劑。LY117018 對(duì)乳腺癌細(xì)胞具有抗增殖作用。靶點(diǎn)
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Estrogen receptor
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體外研究
LY117018 (0.01-1000 nM; 24 hours) at lower concentrations (0.01-10 nM) caused an E2-like increase in p53 levels when compared to its effects on cells grown in the stripped medium. At a higher concentration of LY117018 (1 μM), the level of p53 appeared to decline. Treatment with 1 μM LY117018 resulted in a predominantly hypophosphorylated pRb. At lower concentrations, LY117018 did not block E2-induced pRb phosphorylation.
LY117018 (1 μM; 96 hours) inhibits MCF-7 cells proliferation with an IC
50
of 1 μM.
LY117018 suppresses oxidative stress-induced endothelial cell apoptosis through activation of ERK1/2 signaling pathway.
Cell Proliferation Assay
| Cell Line: | MCF-7 cells |
| Concentration: | 1 μM |
| Incubation Time: | 96 hours |
| Result: | Inhibited MCF-7 cells proliferation with an IC 50 of 1 μM. |